Binimetinib
Vista determinista de la entidad fuente YAML. La autoridad clínica sigue con los ID de fuente citados y estado de firma del revisor.
| ID | DRUG-BINIMETINIB |
|---|---|
| Tipo | Fármaco |
| Aliaces | ARRY-162MEK162- Mektovi.Бінiметиніб |
| Situación | reviewed 2026-04-27 | pending_clinical_signoff |
| Enfermedades | DIS-MELANOMA |
| Fuentes | SRC-ESMO-MELANOMA-2024 SRC-NCCN-MELANOMA-2025 |
Datos sobre drogas
| Clase | Inhibidor MEK1/2 |
|---|---|
| Mecanismo | Selective allosteric (non-ATP-competitive) inhibitor of MEK1/MEK2 kinases that bind a pocket adjacent to the ATP site, locking MEK in an inactive conformation. Blocks downstream phosphorylation of ERK1/2 in the constitutively activated RAS/RAF/MEK/ERK pathway, suppressing proliferation and survival signaling in BRAF V600-mutant tumor cells. Combined with a BRAF inhibitor (encorafenib) the doublet mitigates paradoxical MAPK reactivation seen with BRAFi monotherapy and prolongs response duration. Clinical evidence: COLUMBUS (encorafenib + binimetinib vs vemurafenib in BRAF V600 unresectable / metastatic melanoma, mPFS 14.9 vs 7.3 mo, mOS 33.6 vs 16.9 mo). Historically evaluated as the third agent in BEACON-CRC triplet (no OS gain over encorafenib + cetuximab doublet — doublet is the standard for BRAF V600E mCRC). |
| Dosificación típica | 45 mg PO BID continuo (cada ~ 12 horas), con o sin alimentos, en combinación con encorafenib 450 mg PO una vez al día (programa de COLUMBUS para el melanoma BRAF V600). Modificar la dosis para la insuficiencia hepática (evitar en grado moderado-grave por etiqueta) y para los acontecimientos adversos: nivel de dosis -1 es de 30 mg BID; -2 es interrupción permanente si la toxicidad recurrente del G3-4. |
| Ucrania registrada | Falso |
| NSZU reembolsado | Falso |
| Ucrania verificada por última vez | 2026-04-27 |
Notas
Used exclusively in combination with encorafenib for BRAF V600 melanoma (COLUMBUS) — encorafenib monotherapy is not standard. Mandatory baseline workup: LFTs, CK, LVEF echo, ophthalmologic exam, ECG (for QTc), pregnancy test. Monitor: LFTs + CK every 2 weeks for first 8 weeks then monthly; LVEF echo at 1 month then every 3 months; ophtho for any new visual symptom. Compared with dabrafenib+trametinib the toxicity profile is broadly similar but with less pyrexia and somewhat more retinal events. In UA, access is via cross-border EU centers, EAP, or self-pay; dabrafenib+trametinib remains the НСЗУ-funded BRAFi+MEKi.
Utilizado por
Esquema terapéutico
REG-ENCORAFENIB-BINIMETINIB-MELANOMA- Encorafenib + binimetinib (melanoma BRAF V600E/K)